公开(公告)号：US5389625A

公开(公告)日：1995-02-14

申请号：US849019

申请日：1992-06-08

申请人： Hiroyuki Muro ,  Masayasu Kasai ,  Satoru Hatano ,  Ken-ichi Nishimura ,  Susumu Nishizawa ,  Nobuharu Kakeya

发明人： Hiroyuki Muro ,  Masayasu Kasai ,  Satoru Hatano ,  Ken-ichi Nishimura ,  Susumu Nishizawa ,  Nobuharu Kakeya

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/20 ,  C07D501/22

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.

摘要翻译： PCT No.PCT / JP90 / 01370 Sec。 371日期：1992年6月8日 102（e）日期1992年6月8日PCT 1990年10月24日PCT PCT。 出版物WO91 / 06549 日本1991年5月16日。式（I）r烷基和R 2的头孢菌素化合物是1-烷酰氧基烷基或1-烷氧基羰氧基烷基，其药学上可接受的盐，其制备方法及其药物用途。 头孢菌素化合物及其盐在消化道吸收方面优越，并且在消化道吸收时，作为水解产物在体内表现出广泛的抗微生物活性，此外，它们的甜度比蔗糖高10-400倍 。 因此，所述化合物可用作口服给药以预防和治疗细菌感染性疾病的药剂。

公开(公告)号：US4680413A

公开(公告)日：1987-07-14

申请号：US814893

申请日：1985-12-30

申请人： Yoshikazu Genda ,  Hiroyuki Muro ,  Kiyoharu Nakayama ,  Yoshiaki Miyazaki ,  Yoshiji Sugita

发明人： Yoshikazu Genda ,  Hiroyuki Muro ,  Kiyoharu Nakayama ,  Yoshiaki Miyazaki ,  Yoshiji Sugita

IPC分类号： C07D207/34 ,  C07D405/04 ,  C07D207/22

CPC分类号： C07D405/04 ,  C07D207/34

摘要： A process for the production of a compound having the formula: ##STR1## which comprises a reaction of a compound having the formula: ##STR2## with a compound having the formulaR.sup.2 SO.sub.2 CH.sub.2 NCwhereinX is same or different substituent(s) selected from the group consisting of halogen, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, C.sub.1-6 alkylamino, C.sub.1-6 alkoxy, nitro, cyano and methylenedioxy;COOR.sup.1 is carboxylic acid or ester;R.sup.2 is C.sub.1-10 cyclic hydrocarbon which may be substituted by substituent(s) not giving negative effects to said reaction;n is 0, 1 or 2.

摘要翻译： 制备具有下式的化合物的方法：包括具有下式的化合物与下式的化合物的反应：其中X是相同或不同的选自下列基团的取代基： 由卤素，C 1-6烷基，C 1-6卤代烷基，C 1-6烷基氨基，C 1-6烷氧基，硝基，氰基和亚甲二氧基组成。 COOR1是羧酸或酯; R2是可以被不对所述反应产生负面影响的取代基取代的C1-10环烃; n为0,1或2。

公开(公告)号：US4943567A

公开(公告)日：1990-07-24

申请号：US228714

申请日：1988-05-27

申请人： Susumu Nishizawa ,  Hiroyuki Muro ,  Masayasu Kasai ,  Satoru Hatano ,  Syouzi Kamiya ,  Nobuharu Kakeya ,  Kazuhiko Kitao

发明人： Susumu Nishizawa ,  Hiroyuki Muro ,  Masayasu Kasai ,  Satoru Hatano ,  Syouzi Kamiya ,  Nobuharu Kakeya ,  Kazuhiko Kitao

IPC分类号： C07D277/20 ,  C07D277/38 ,  C07D285/08 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D277/587 ,  C07D285/08 ,  Y02P20/55

摘要： Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.